ES2803028T3 - Partículas de n-(5-ciano-4-((2-metoxietil)amino)piridin-2-il)-7-formil-6-((4-metil-2-oxopiperazin-1-il)metil)-3,4-dihidro-1,8-naftiridin-1(2h)-carboxamida - Google Patents
Partículas de n-(5-ciano-4-((2-metoxietil)amino)piridin-2-il)-7-formil-6-((4-metil-2-oxopiperazin-1-il)metil)-3,4-dihidro-1,8-naftiridin-1(2h)-carboxamida Download PDFInfo
- Publication number
- ES2803028T3 ES2803028T3 ES16712082T ES16712082T ES2803028T3 ES 2803028 T3 ES2803028 T3 ES 2803028T3 ES 16712082 T ES16712082 T ES 16712082T ES 16712082 T ES16712082 T ES 16712082T ES 2803028 T3 ES2803028 T3 ES 2803028T3
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- Prior art keywords
- methyl
- particles
- citric acid
- carboxamide
- dihydro
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- 239000005720 sucrose Substances 0.000 description 1
- 239000000829 suppository Substances 0.000 description 1
- 239000004094 surface-active agent Substances 0.000 description 1
- 230000002459 sustained effect Effects 0.000 description 1
- 238000003786 synthesis reaction Methods 0.000 description 1
- 239000006188 syrup Substances 0.000 description 1
- 235000020357 syrup Nutrition 0.000 description 1
- GKVCSXCAXPSOKK-UHFFFAOYSA-N tert-butyl N-(4-chloro-5-cyanopyridin-2-yl)carbamate Chemical compound CC(C)(C)OC(=O)Nc1cc(Cl)c(cn1)C#N GKVCSXCAXPSOKK-UHFFFAOYSA-N 0.000 description 1
- GKWGBMHXVRSFRT-UHFFFAOYSA-N tert-butyl n-[2-(methylamino)ethyl]carbamate Chemical compound CNCCNC(=O)OC(C)(C)C GKWGBMHXVRSFRT-UHFFFAOYSA-N 0.000 description 1
- CZDYPVPMEAXLPK-UHFFFAOYSA-N tetramethylsilane Chemical compound C[Si](C)(C)C CZDYPVPMEAXLPK-UHFFFAOYSA-N 0.000 description 1
- 238000010257 thawing Methods 0.000 description 1
- 239000000196 tragacanth Substances 0.000 description 1
- 235000010487 tragacanth Nutrition 0.000 description 1
- 229940116362 tragacanth Drugs 0.000 description 1
- 238000012546 transfer Methods 0.000 description 1
- PQDJYEQOELDLCP-UHFFFAOYSA-N trimethylsilane Chemical compound C[SiH](C)C PQDJYEQOELDLCP-UHFFFAOYSA-N 0.000 description 1
- RYFMWSXOAZQYPI-UHFFFAOYSA-K trisodium phosphate Chemical compound [Na+].[Na+].[Na+].[O-]P([O-])([O-])=O RYFMWSXOAZQYPI-UHFFFAOYSA-K 0.000 description 1
- 238000004704 ultra performance liquid chromatography Methods 0.000 description 1
- 241001430294 unidentified retrovirus Species 0.000 description 1
- 238000011179 visual inspection Methods 0.000 description 1
- 238000001262 western blot Methods 0.000 description 1
- 239000000080 wetting agent Substances 0.000 description 1
- 229910052725 zinc Inorganic materials 0.000 description 1
- 239000011701 zinc Substances 0.000 description 1
- GTLDTDOJJJZVBW-UHFFFAOYSA-N zinc cyanide Chemical compound [Zn+2].N#[C-].N#[C-] GTLDTDOJJJZVBW-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
- A61K31/4375—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/08—Drugs for disorders of the urinary system of the prostate
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C51/00—Preparation of carboxylic acids or their salts, halides or anhydrides
- C07C51/41—Preparation of salts of carboxylic acids
- C07C51/412—Preparation of salts of carboxylic acids by conversion of the acids, their salts, esters or anhydrides with the same carboxylic acid part
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C59/00—Compounds having carboxyl groups bound to acyclic carbon atoms and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups
- C07C59/235—Saturated compounds containing more than one carboxyl group
- C07C59/245—Saturated compounds containing more than one carboxyl group containing hydroxy or O-metal groups
- C07C59/265—Citric acid
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/13—Crystalline forms, e.g. polymorphs
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Oil, Petroleum & Natural Gas (AREA)
- Epidemiology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Neurology (AREA)
- Physical Education & Sports Medicine (AREA)
- Pulmonology (AREA)
- Endocrinology (AREA)
- Reproductive Health (AREA)
- Gastroenterology & Hepatology (AREA)
- Urology & Nephrology (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2015000202 | 2015-03-25 | ||
| PCT/IB2016/051633 WO2016151500A1 (en) | 2015-03-25 | 2016-03-23 | Particles of n-(5-cyano-4-((2-methoxyethyl)amino)pyridin-2-yl)-7-formyl-6-((4-methyl-2- oxopiperazin-1-yl)methyl)-3,4-dihydro-1,8-naphthyridine-1(2h)-carboxamide |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ES2803028T3 true ES2803028T3 (es) | 2021-01-22 |
Family
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES16712082T Active ES2803028T3 (es) | 2015-03-25 | 2016-03-23 | Partículas de n-(5-ciano-4-((2-metoxietil)amino)piridin-2-il)-7-formil-6-((4-metil-2-oxopiperazin-1-il)metil)-3,4-dihidro-1,8-naftiridin-1(2h)-carboxamida |
Country Status (14)
| Country | Link |
|---|---|
| US (1) | US9802917B2 (enExample) |
| EP (1) | EP3274349B1 (enExample) |
| JP (1) | JP6696995B2 (enExample) |
| KR (1) | KR102606643B1 (enExample) |
| CN (1) | CN107406448B (enExample) |
| AR (1) | AR104060A1 (enExample) |
| AU (2) | AU2016238437B2 (enExample) |
| CA (1) | CA2977326C (enExample) |
| ES (1) | ES2803028T3 (enExample) |
| MX (1) | MX2017012293A (enExample) |
| PL (1) | PL3274349T3 (enExample) |
| RU (1) | RU2720456C2 (enExample) |
| TW (1) | TWI699206B (enExample) |
| WO (1) | WO2016151500A1 (enExample) |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| WO2016054483A1 (en) * | 2014-10-03 | 2016-04-07 | Novartis Ag | Use of ring-fused bicyclic pyridyl derivatives as fgfr4 inhibitors |
| CN113105454B (zh) * | 2016-05-20 | 2022-10-11 | 江苏豪森药业集团有限公司 | Fgfr4抑制剂、其制备方法和应用 |
| CN107619388A (zh) | 2016-07-13 | 2018-01-23 | 南京天印健华医药科技有限公司 | 作为fgfr抑制剂的杂环化合物 |
| CA3075720A1 (en) * | 2017-10-02 | 2019-04-11 | Novartis Ag | Method for preparing a pharmaceutical product |
| CN110234649B (zh) * | 2017-10-31 | 2021-10-15 | 江苏豪森药业集团有限公司 | Fgfr4抑制剂的盐、晶体、制备方法及其用途 |
| CN110225913B (zh) * | 2017-10-31 | 2021-10-15 | 江苏豪森药业集团有限公司 | Fgfr4抑制剂晶型及其制备方法 |
| CN109745321B (zh) * | 2017-11-08 | 2022-04-29 | 上海翰森生物医药科技有限公司 | 包含fgfr4抑制剂的药物组合物 |
| WO2020257527A1 (en) * | 2019-06-21 | 2020-12-24 | Terns, Inc. | Compounds for inhibiting fgfr4 |
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| GB9420999D0 (en) | 1994-10-18 | 1994-12-07 | Smithkline Beecham Plc | Novel compounds |
| WO1998004554A1 (en) | 1996-07-29 | 1998-02-05 | Banyu Pharmaceutical Co., Ltd. | Chemokine receptor antagonists |
| WO1999031061A1 (en) | 1997-12-17 | 1999-06-24 | Merck & Co., Inc. | Integrin receptor antagonists |
| AR015514A1 (es) | 1998-02-10 | 2001-05-02 | Novartis Ag | Compuesto de amida, proceso para su preparacion y composicion farmaceutica que lo contiene |
| US7115750B1 (en) | 1999-09-20 | 2006-10-03 | Takeda Pharmaceutical Company Limited | Melanin concentrating hormone antagonist |
| AU2003211951A1 (en) | 2002-02-14 | 2003-09-04 | Ono Pharmaceutical Co., Ltd. | N-carbamoyl nitrogen-containing fused ring compounds and drugs containing these compounds as the active ingredient |
| AU2003252478A1 (en) | 2002-07-10 | 2004-02-02 | Ono Pharmaceutical Co., Ltd. | Ccr4 antagonist and medicinal use thereof |
| AU2003303231A1 (en) | 2002-12-20 | 2004-07-14 | Warner-Lambert Company Llc | Benzoxazines and derivatives thereof as inhibitors of pi3ks |
| US7098332B2 (en) * | 2002-12-20 | 2006-08-29 | Hoffmann-La Roche Inc. | 5,8-Dihydro-6H-pyrido[2,3-d]pyrimidin-7-ones |
| WO2004080966A1 (ja) | 2003-03-14 | 2004-09-23 | Ono Pharmaceutical Co., Ltd. | 含窒素複素環誘導体およびそれらを有効成分とする薬剤 |
| US7183413B2 (en) | 2003-04-11 | 2007-02-27 | Taigen Biotechnology | Aminoquinoline compounds |
| MXPA06002853A (es) | 2003-09-11 | 2006-06-14 | Kemia Inc | Inhibidores citoquina. |
| EP1907388A1 (en) | 2005-07-15 | 2008-04-09 | F. Hoffmann-Roche AG | Novel heteroaryl fused cyclic amines |
| WO2007071752A2 (en) | 2005-12-21 | 2007-06-28 | Novartis Ag | Pyrimidinyl aryl urea derivatives being fgf inhibitors |
| CA2635845A1 (en) | 2005-12-29 | 2007-07-12 | Janssen Pharmaceutica N.V. | Prokineticin 2 receptor antagonists |
| WO2007105637A1 (ja) | 2006-03-10 | 2007-09-20 | Ono Pharmaceutical Co., Ltd. | 含窒素複素環誘導体およびそれらを有効成分とする薬剤 |
| WO2007146230A2 (en) | 2006-06-14 | 2007-12-21 | Merck & Co., Inc. | Non-nucleoside reverse transcriptase inhibitors |
| RU2009136669A (ru) | 2007-03-09 | 2011-04-20 | Новартис АГ (CH) | Лечение меланомы |
| JP2011507848A (ja) | 2007-12-21 | 2011-03-10 | ザ スクリプス リサーチ インスティチュート | Ｒｈｏキナーゼインヒビターとしてのベンゾピランおよびアナログ |
| US20110172217A1 (en) | 2008-09-05 | 2011-07-14 | Shionogi & Co., Ltd. | Ring-fused morpholine derivative having pi3k-inhibiting activity |
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| GB0906472D0 (en) | 2009-04-15 | 2009-05-20 | Astex Therapeutics Ltd | New compounds |
| MX2011011735A (es) | 2009-05-04 | 2011-11-29 | Plexxikon Inc | Compuestos y metodos para la inhibicion de renina, e indicaciones para ello. |
| US9556201B2 (en) | 2009-10-29 | 2017-01-31 | Glaxosmithkline Llc | Bicyclic pyridines and analogs as sirtuin modulators |
| ES2524548T3 (es) | 2009-10-30 | 2014-12-10 | Novartis Ag | N-óxido de 3-(2,6-dicloro-3,5-dimetoxi-fenil)-1-{6-[4-(4-etil-piperacin-1-il)-fenilamino]-pirimidin-4-il}-1-metil-urea |
| JPWO2011093501A1 (ja) | 2010-02-01 | 2013-06-06 | 日本ケミファ株式会社 | Ｇｐｒ１１９作動薬 |
| WO2011111880A1 (ko) | 2010-03-08 | 2011-09-15 | 주식회사 메디젠텍 | 세포핵에서 세포질로의 ｇｓｋ３의 이동을 억제하는 화합물을 함유하는 세포핵에서 세포질로의 gsk3 이동에 의해 발생되는 질환의 치료 또는 예방용 약학적 조성물 |
| KR101764952B1 (ko) | 2010-07-29 | 2017-08-03 | 리겔 파마슈티칼스, 인크. | Ａｍｐｋ-활성화 헤테로시클릭 화합물 및 그의 사용 방법 |
| JP5620417B2 (ja) * | 2011-02-07 | 2014-11-05 | 中外製薬株式会社 | アミノピラゾール誘導体を含む医薬 |
| AP2013007153A0 (en) | 2011-03-18 | 2013-09-30 | Lupin Ltd | Benzo [B] [1,4] oxazin derivatives as calcium sensing receptor modulators |
| GB201118656D0 (en) | 2011-10-28 | 2011-12-07 | Astex Therapeutics Ltd | New compounds |
| NZ703495A (en) | 2012-07-11 | 2018-02-23 | Blueprint Medicines Corp | Inhibitors of the fibroblast growth factor receptor |
| US9315519B2 (en) | 2012-10-12 | 2016-04-19 | Bristol-Myers Squibb Company | Guanidine substituted tetrahydroisoquinoline compounds as factor XIa inhibitors |
| WO2014059214A1 (en) | 2012-10-12 | 2014-04-17 | Bristol-Myers Squibb Company | Guanidine and amine substituted tetrahydroisoquinoline compounds as factor xia inhibitors |
| WO2014079709A1 (en) | 2012-11-23 | 2014-05-30 | Ab Science | Use of small molecule inhibitors/activators in combination with (deoxy)nucleoside or (deoxy)nucleotide analogs for treatment of cancer and hematological malignancies or viral infections |
| JP6576325B2 (ja) | 2013-03-15 | 2019-09-18 | セルジーン シーエーアール エルエルシー | ヘテロアリール化合物およびそれらの使用 |
| LT2986610T (lt) | 2013-04-19 | 2018-04-10 | Incyte Holdings Corporation | Bicikliniai heterociklai, kaip fgfr inhibitoriai |
| GB201307577D0 (en) | 2013-04-26 | 2013-06-12 | Astex Therapeutics Ltd | New compounds |
| AU2014287209B2 (en) | 2013-07-09 | 2019-01-24 | Dana-Farber Cancer Institute, Inc. | Kinase inhibitors for the treatment of disease |
| AR097455A1 (es) | 2013-08-28 | 2016-03-16 | Astellas Pharma Inc | Composición farmacéutica que contiene compuesto de pirimidina como un ingrediente activo |
| SMT201800379T1 (it) | 2013-10-18 | 2018-09-13 | Eisai R&D Man Co Ltd | Inibitori di fgfr4 della pirimidina |
| BR112016008276B1 (pt) | 2013-10-25 | 2021-03-02 | Novartis Ag | derivados bicíclicos de piridila fundidos ao anel, seus usos e seu intermediário, e composição farmacêutica |
| DK3395814T3 (da) | 2013-10-25 | 2022-07-04 | Blueprint Medicines Corp | Hæmmere af fibroblastvækstfaktorreceptoren |
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2016
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- 2016-03-23 PL PL16712082T patent/PL3274349T3/pl unknown
- 2016-03-23 ES ES16712082T patent/ES2803028T3/es active Active
- 2016-03-23 AU AU2016238437A patent/AU2016238437B2/en active Active
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- 2016-03-23 CA CA2977326A patent/CA2977326C/en active Active
- 2016-03-23 JP JP2017549754A patent/JP6696995B2/ja active Active
- 2016-03-23 WO PCT/IB2016/051633 patent/WO2016151500A1/en not_active Ceased
- 2016-03-23 AR ARP160100792A patent/AR104060A1/es unknown
- 2016-03-23 KR KR1020177026470A patent/KR102606643B1/ko active Active
- 2016-03-23 CN CN201680018234.6A patent/CN107406448B/zh active Active
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- 2016-03-23 RU RU2017133243A patent/RU2720456C2/ru active
- 2016-03-24 TW TW105109283A patent/TWI699206B/zh active
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2019
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Also Published As
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|---|---|
| TWI699206B (zh) | 2020-07-21 |
| EP3274349B1 (en) | 2020-04-22 |
| AU2016238437B2 (en) | 2018-11-08 |
| US9802917B2 (en) | 2017-10-31 |
| AU2019200936A1 (en) | 2019-02-28 |
| PL3274349T3 (pl) | 2020-10-05 |
| RU2017133243A3 (enExample) | 2019-07-29 |
| KR20170129758A (ko) | 2017-11-27 |
| CA2977326A1 (en) | 2016-09-29 |
| EP3274349A1 (en) | 2018-01-31 |
| AU2016238437A1 (en) | 2017-08-17 |
| CA2977326C (en) | 2023-08-29 |
| RU2720456C2 (ru) | 2020-04-30 |
| CN107406448A (zh) | 2017-11-28 |
| MX2017012293A (es) | 2018-01-09 |
| BR112017016991A2 (pt) | 2018-04-10 |
| KR102606643B1 (ko) | 2023-11-28 |
| WO2016151500A1 (en) | 2016-09-29 |
| TW201641106A (zh) | 2016-12-01 |
| US20160304489A1 (en) | 2016-10-20 |
| RU2017133243A (ru) | 2019-04-05 |
| AR104060A1 (es) | 2017-06-21 |
| JP2018509446A (ja) | 2018-04-05 |
| JP6696995B2 (ja) | 2020-05-20 |
| CN107406448B (zh) | 2021-03-09 |
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